N1-(3,5-dichloropyrid-4-yl)-4-difluoromethoxy-8-amino-dibenzo[b,d]furan-1-carboxamide | 685875-03-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并呋喃
• 英文名称: N1-(3,5-dichloropyrid-4-yl)-4-difluoromethoxy-8-amino-dibenzo[b,d]furan-1-carboxamide
• 英文别名: N-(3,5-dichloropyridin-4-yl)-4-difluoromethoxy-8-aminodibenzo[b,d]furan-1-carboxamide；N-(3,5-dichloropyrid-4-yl)-4-difluoromethoxy-8-amino-dibenzo[b,d]furan-1-carboxamide；8-amino-N-(3,5-dichloropyridin-4-yl)-4-(difluoromethoxy)dibenzofuran-1-carboxamide
• CAS: 685875-03-0
• 化学式: C₁₉H₁₁Cl₂F₂N₃O₃
• 分子量: 438.217
• InChiKey: OVZIMKLJOOFNQJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.9
• 重原子数：
  29
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.05
• 拓扑面积：
  90.4
• 氢给体数：
  2
• 氢受体数：
  7

反应信息

• 作为反应物：
  描述：

  N1-(3,5-dichloropyrid-4-yl)-4-difluoromethoxy-8-amino-dibenzo[b,d]furan-1-carboxamide 生成 N-(3,5-二氯吡啶-4-基)-4-二氟甲氧基-8-[(甲磺酰基)氨基]二苯并[B,D]呋喃-1-甲酰胺
  参考文献：
  名称：

  [EN] PROCESS FOR THE PREPARATION OF N-(3,5-DICHLOROPYRID-4-YL)-4DIFLUOROMETHOXY-8-METHANESULFONAMIDO-DIBENZO[B,D]FURAN-1-CARBOXAMIDE
  [FR] PROCEDE DE PREPARATION DE N-(3,5-DICHLOROPYRID-4-YL)-4-DIFLUOROMETHOXY-8-METHANESULFONAMIDO-DIBENZO[B,D]FURAN-1-CARBOXAMIDE

  摘要：

  本发明涉及制备N-(3,5-二氯吡啶-4-基)-4-二氟甲氧基-8-甲磺酰基-二苯并[b,d]呋喃-1-羧酰胺及其药学上可接受的盐，如其钠盐，以及在合成上述化合物中有用的新的中间体化合物的方法。

  公开号：

  WO2006040652A2
• 作为产物：
  描述：

  N-(3,5-dichloro-pyridin-4-yl)-4-difluoromethoxy-8-nitro-dibenzo[b,d]furane-1-carboxamide 在 钯 甲醇 作用下， 以 甲醇 为溶剂， 反应 12.0h， 以afforded N-(3,5-dichloropyrid-4-yl)-4-difluoromethoxy-8-amino-dibenzo[b,d]furan-1-carboxamide as white solid的产率得到N1-(3,5-dichloropyrid-4-yl)-4-difluoromethoxy-8-amino-dibenzo[b,d]furan-1-carboxamide
  参考文献：
  名称：

  NOVEL HETEROCYCLIC COMPOUNDS USEFUL FOR THE TREATMENT OF INFLAMMATORY AND ALLERGIC DISORDERS: PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

  摘要：

  本发明涉及新型杂环化合物及其类似物、互变异构体、位置异构体、立体异构体、对映异构体、非对映异构体、多型体、药学上可接受的盐、适当的N-氧化物、药学上可接受的溶剂和包含它们的药物组合物。本发明更特别涉及式（1）的新型磷酸二酯酶4（PDE4）抑制剂及其类似物、互变异构体、对映异构体、非对映异构体、位置异构体、立体异构体、多型体、药学上可接受的盐、适当的N-氧化物、药学上可接受的溶剂和包含它们的药物组合物。

  公开号：

  US20070105854A1

文献信息

• [EN] NOVEL TRICYCLIC COMPOUNDS USEFUL FOR THE TREATMENT OF INFLAMMATORY AND ALLERGIC DISORDERS: PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM<br/>[FR] NOUVEAUX COMPOSES TRICYCLIQUES UTILES POUR TRAITER LES TROUBLES INFLAMMATOIRES ET ALLERGIQUES, PROCEDE DE PREPARATION DE CES COMPOSES ET COMPOSITIONS PHARMACEUTIQUES LES CONTENANT
  申请人：GLENMARK PHARMACEUTICALS LTD

  公开号：WO2004037805A1

  公开（公告）日：2004-05-06

  The present invention relates to novel tricyclic compounds useful for the treatment of inflammatory conditions, diseases of the central nervous and insulin resistant diabetes.

  本发明涉及用于治疗炎症性疾病、中枢神经系统疾病和胰岛素抵抗性糖尿病的新型三环化合物。
• [EN] NOVEL HETEROCYCLIC COMPOUNDS USEFUL FOR THE TREATMENT OF INFLAMMATORY AND ALLERGIC DISORDERS: PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM<br/>[FR] NOUVEAUX COMPOSES HETEROCYCLIQUES POUR LE TRAITEMENT DES AFFECTIONS INFLAMMATOIRES ET ALLERGIQUES, LEUR PROCEDE DE PREPARATION ET COMPOSITIONS PHARMACEUTIQUES LES CONTENANT
  申请人：GLENMARK PHARMACEUTICALS LTD

  公开号：WO2004089940A1

  公开（公告）日：2004-10-21

  The present invention relates to novel heterocyclic compounds, their analogs, their tautomers, their regioisomers, their stereoisomers, their enantiomers, their diastereomers, their polymorphs, their pharmaceutically acceptable salts, their appropriate N-oxides, their pharmaceutically acceptable solvates and their pharmaceutical compositions containing them. The present invention more particularly relates to novel Phosphodiesterase type 4 (PDE4) inhibitors of the formula (1), their analogs, their tautomers, their enantiomers, their diasteromers, their regioisomers, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their appropriate N-oxide, their pharmaceutically acceptable solvates and the pharmaceutical compositions containing them. The groups X, Ar, Y, P and R1-R4 are defined in claim 1.

  本发明涉及新颖的杂环化合物，它们的类似物，其互变异构体，其位置异构体，其立体异构体，其对映异构体，其二对映异构体，其多晶形式，其药用可接受盐，其适当的N-氧化物，其药用可接受溶剂和含有它们的药物组合物。本发明更具体地涉及公式（1）的新型磷酸二酯酶4型（PDE4）抑制剂，其类似物，其互变异构体，其对映异构体，其二对映异构体，其位置异构体，其立体异构体，其多晶形式，其药用可接受盐，其适当的N-氧化物，其药用可接受溶剂和含有它们的药物组合物。其中，X、Ar、Y、P 和 R1-R4 组在权利要求书中有定义。
• SYNTHESIS OF HETEROCYCLIC COMPOUNDS
  申请人：Araldi Gian-Luca

  公开号：US20080009632A1

  公开（公告）日：2008-01-10

  Methods for the synthesis of heterocyclic compounds including N-(3,5-dichloropyrid-4-yl)-4-difluoromethoxy-8-methanesulfonamido-dibenzo[b,d]furan-1-carboxamide and pharmaceutically acceptable salts thereof.

  合成杂环化合物的方法，包括N-(3,5-二氯吡啶-4-基)-4-二氟甲氧基-8-甲磺酰氨基-二苯并[b,d]呋喃-1-羧酰胺及其药用盐。
• Heterocyclic compounds useful for the treatment of inflammatory and allergic disorders
  申请人：Glenmark Pharmaceuticals, S.A.

  公开号：US07393846B2

  公开（公告）日：2008-07-01

  The present invention relates to novel heterocyclic compounds, their analogs, their tautomers, their regioisomers, their stereoisomers, their enantiomers, their diastereomers, their polymorphs, their pharmaceutically acceptable salts, their appropriate N-oxides, their pharmaceutically acceptable solvates and their pharmaceutical compositions containing them. The present invention more particularly relates to novel Phosphodiesterase type 4 (PDE4) inhibitors of the Formula (1), their analogs, tautomers, enantiomers, diasteromers, regioisomers, stereoisomers, polymorphs, pharmaceutically acceptable salts, appropriate N-oxide, pharmaceutically acceptable solvates and the pharmaceutical compositions containing them.

  本发明涉及新型杂环化合物及其类似物、互变异构体、位置异构体、立体异构体、对映异构体、二对映异构体、多晶型、药学上可接受的盐、适当的N-氧化物、药学上可接受的溶剂化物和含有它们的制药组合物。本发明更具体地涉及公式（1）的新型磷酸二酯酶4（PDE4）抑制剂及其类似物、互变异构体、对映异构体、二对映异构体、位置异构体、立体异构体、多晶型、药学上可接受的盐、适当的N-氧化物、药学上可接受的溶剂化物和含有它们的制药组合物。
• Process for the preparation n-(3,5-dichloropyrid-4-yl)-4-difluoromethoxy-8-methane sulfonamido-dibenzo[b,d]furan-1-carboxamide
  申请人：Gopalan Balasubramanian

  公开号：US20060135779A1

  公开（公告）日：2006-06-22

  The present invention relates to a method of preparing N-(3,5-dichloropyrid-4-yl)-4-difluoromethoxy-8-methanesulfonamido-dibenzo[b,d]furan-1-carboxamide and pharmaceutically acceptable salts thereof, such as its sodium salt, and novel intermediate compounds useful in the synthesis of the aforementioned compound.

  本发明涉及一种制备N-（3,5-二氯吡啶-4-基）-4-二氟甲氧基-8-甲磺酰氨基-二苯并[b,d]呋喃-1-羧酰胺及其药学上可接受的盐，例如其钠盐，以及在合成上述化合物中有用的新型中间体化合物的方法。